Identification
- Generic Name
- AP5346
- DrugBank Accession Number
- DB04992
- Background
AP5346 is designed to target a diaminocyclohexane platinum (Pt) moiety to tumors through pH-sensitive linkage to a 25 kDa hydroxypropylmethacrylamide polymer. It is being pursued by Access Pharmaceuticals, Inc.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
- External IDs
- AP5346
Pharmacology
- Indication
For the treatment of various forms of cancer.
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Preclinical studies of the delivery of platinum to tumors in an animal model has shown that, compared with oxaliplatin at equitoxic doses, AP5346 delivers in excess of 16 times more platinum to the tumor. An analysis of tumor DNA, which is the main target for anti-cancer platinum agents, has shown that in excess of 13 times more platinum tumor DNA complexes were formed from AP5346 than oxaliplatin in these studies. Results from preclinical efficacy studies conducted in the B16 and other tumor models have also shown that AP5346 is superior to oxaliplatin in inhibiting the growth of tumors.
- Mechanism of action
Utilizing the biocompatible water-soluble polymer HPMA as a drug carrier, AP5346 links DACH platinum to the polymer in a manner which permits the selective release of platinum in tumors. The polymer capitalizes on the biological differences in the permeability of blood vessels at tumor sites versus normal tissue. In this way, tumor selective delivery and platinum release is achieved. Once delivered to the tumor, platinum binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and function.
Target Actions Organism UDNA Not Available Humans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Products
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- ProLindac
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Not Available
- CAS number
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Rice JR, Gerberich JL, Nowotnik DP, Howell SB: Preclinical efficacy and pharmacokinetics of AP5346, a novel diaminocyclohexane-platinum tumor-targeting drug delivery system. Clin Cancer Res. 2006 Apr 1;12(7 Pt 1):2248-54. [Article]
- Campone M, Rademaker-Lakhai JM, Bennouna J, Howell SB, Nowotnik DP, Beijnen JH, Schellens JH: Phase I and pharmacokinetic trial of AP5346, a DACH-platinum-polymer conjugate, administered weekly for three out of every 4 weeks to advanced solid tumor patients. Cancer Chemother Pharmacol. 2007 Sep;60(4):523-33. Epub 2007 Feb 17. [Article]
- Sood P, Thurmond KB 2nd, Jacob JE, Waller LK, Silva GO, Stewart DR, Nowotnik DP: Synthesis and characterization of AP5346, a novel polymer-linked diaminocyclohexyl platinum chemotherapeutic agent. Bioconjug Chem. 2006 Sep-Oct;17(5):1270-9. [Article]
- Van der Schoot SC, Nuijen B, Sood P, Thurmond KB 2nd, Stewart DR, Rice JR, Beijnen JH: Pharmaceutical development, quality control, stability and compatibility of a parenteral lyophilized formulation of the investigational polymer-conjugated platinum antineoplastic agent AP5346. Pharmazie. 2006 Oct;61(10):835-44. [Article]
- External Links
- PubChem Substance
- 347909880
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count Not Available Unknown Status Treatment Head And Neck Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
Drug created at October 21, 2007 22:23 / Updated at June 12, 2020 16:52